Synthesis and biological evaluation of a 5-6-5 imidazole-phenyl-thiazole based α-helix mimetic

Christopher G. Cummings, Nathan T. Ross, William P. Katt, Andrew D. Hamilton

Research output: Contribution to journalArticlepeer-review

Abstract

The development of small molecules that disrupt protein-protein interactions is a key goal in addressing a number of disease states. The α-helix is commonly found at protein interaction interfaces and has been the focus of substantial small molecule mimetic efforts. One of the primary drawbacks of many small molecule α-helix mimetics is their hydrophobic core structures. To address this problem we have developed a novel scaffold based on a more water soluble 5-6-5 imidazole-phenyl-thiazole core. An inhibitor of this class has been shown to disrupt the Cdc42/Dbs protein-protein interaction at micromolar concentrations and may be useful in overcoming Cdc42-induced tumor resistance to anticancer therapies.

Original languageEnglish (US)
Pages (from-to)25-28
Number of pages4
JournalOrganic Letters
Volume11
Issue number1
DOIs
StatePublished - Jan 1 2009

ASJC Scopus subject areas

  • Biochemistry
  • Physical and Theoretical Chemistry
  • Organic Chemistry

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